| 产品描述: | CARM1抑制剂;CARM1 Inhibitors;;InformationSGC2085 SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.TargetsCARM1 (Cell-free assay) 50 nMIn vitroWith the exception of PRMT6 (IC50 = 5.2 μM), SGC2085 does not inhibit other PRMTs. Although CARM1(PRMT4) is previously shown to asymmetrically dimethylate BAF155 at R1064, no cellular activity is observed for SGC2085 when tested up to 10 μM. The absence of cellular activity for SGC2085 may due to poor permeability.Cell Research(from reference)Cell lines:HEK293 cells Concentrations:up to 10 μM Incubation Time:48 h |
| 体内研究: |
SGC2085 (1 μM, 10 μM, 50 μM;48 h) 对 21 种人类蛋白质甲基转移酶的具有完全选择性。 SGC2085 (10 μM;48 h) 表现出低细胞渗透性,在 HEK293 细胞中无细胞活性。 |
| 参考文献: |
1. Ferreira de Freitas R, et al. Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening. J Med Chem. 2016 Jul 28;59(14):6838-47. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.201 ml |
16.005 ml |
32.009 ml |
| 5 mM |
0.64 ml |
3.201 ml |
6.402 ml |
| 10 mM |
0.32 ml |
1.6 ml |
3.201 ml |
| 50 mM |
0.064 ml |
0.32 ml |
0.64 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |